Protein binding influences the bioavailability and distribution of active compounds, and is a limiting factor in the passage of drugs across biological membranes and barriers: drugs are often unable to cross membranes mainly due to the high molecular mass of the drug-protein complex, thus resulting in the accumulation …

Does protein binding affect drug absorption?

Protein-binding may affect drug activity in one of two ways: either by changing the effective concentration of the drug at its site of action or by changing the rate at which the drug is eliminated, thus affecting the length of time for which effective concentrations are maintained.

What is the significance of protein binding?

Protein binding is most clinically significant for antimicrobial therapy, where a high degree of protein binding serves as a drug “depot,” allowing for increased duration of the time the drug concentration remains above the bacterial minimum inhibitory concentration, adding to antimicrobial efficacy.